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    • 7. 发明申请
    • GYRASE INHIBITORS
    • GYRASE抑制剂
    • WO2011032050A2
    • 2011-03-17
    • PCT/US2010/048538
    • 2010-09-10
    • TRIUS THERAPEUTICS, INC.CREIGHTON, ChrisTARI, LesCHEN, ZhiyongHILGERS, MarkLAM, ThanhLI, XiaomingTRZOSS, MichaelZHANG, JunhuFINN, John
    • CREIGHTON, ChrisTARI, LesCHEN, ZhiyongHILGERS, MarkLAM, ThanhLI, XiaomingTRZOSS, MichaelZHANG, JunhuFINN, John
    • C07D487/04C07D519/00A61K31/519A61P31/00
    • C07D519/00C07D471/04C07D471/16C07D487/04C07D487/16C07D491/048C07D513/04
    • Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR 5 ; R 5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR 7 , or CR 8 R 9 ; R 7 is H or C 1-3 alkyl; R 8 and R 9 are each independently H or C 1-3 alkyl; R 2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R 4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0- 12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R 5 and R 4 together may join to form a fused ring; and R 6 is selected from the group consisting of H, C 1-5 alkyl, C 2-5 alkenyl, C 2-5 alkynyl, halo C 1-5 alkyl, halo C 2-5 alkenyl, halo C 2-5 alkynyl, C 1-5 hydroxyalkyl, C 1-5 alkyl chloride, C 2-5 alkenyl chloride, and C 2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.
    • 新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。 公开了式(I)的化合物:式(I),其中Y是N或CH; Z为N或CR5; R5是H,含有0-2个选自O,S和N的杂原子的取代或未取代的烃基残基(1-3C),或是无机残基; L是O,S,NR7或CR8R9; R7是H或C1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H,含有0-10个选自O,S和N的杂原子的烃基残基(1-40℃),任选被无机残基取代; R4是H,无机残基,或含有0-12个选自O,S和N的杂原子并含有0-10个无机残基的烃基残基(1-30℃),其中R 5和R 4可以连接形成稠环; 并且R 6选自H,C 1-5烷基,C 2-5烯基,C 2-5炔基,卤代C 1-5烷基,卤素C 2-5烯基,卤代C 2-5炔基,C 1-5羟基烷基,C 1 -5烷基氯,C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐,酯或前药。